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Issue 11, 2017
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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors

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Abstract

Myeloperoxidase, a mammalian peroxidase involved in the immune system as an anti-microbial first responder, can produce hypochlorous acid in response to invading pathogens. Myeloperoxidase has been implicated in several chronic pathological diseases due to the chronic production of hypochlorous acid, as well as other reactive radical species. A high throughput screen and triaging protocol was developed to identify a reversible inhibitor of myeloperoxidase toward the potential treatment of chronic diseases such as atherosclerosis. The identification and characterization of a reversible myeloperoxidase inhibitor, 7-(benzyloxy)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine is described.

Graphical abstract: Triazolopyrimidines identified as reversible myeloperoxidase inhibitors

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Publication details

The article was received on 24 May 2017, accepted on 05 Oct 2017 and first published on 26 Oct 2017


Article type: Research Article
DOI: 10.1039/C7MD00268H
Citation: Med. Chem. Commun., 2017,8, 2093-2099
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    Triazolopyrimidines identified as reversible myeloperoxidase inhibitors

    F. Duclos, L. M. Abell, D. G. Harden, K. Pike, K. Nowak, G. A. Locke, G. J. Duke, X. Liu, G. Fernando, S. A. Shaw, B. P. Vokits, N. R. Wurtz, A. Viet, M. N. Valente, S. Stachura, P. Sleph, J. A. Khan, J. Gao, A. R. Dongre, L. Zhao, R. R. Wexler, D. A. Gordon and E. K. Kick, Med. Chem. Commun., 2017, 8, 2093
    DOI: 10.1039/C7MD00268H

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